G protein coupled receptors (GPCRs) are key drug targets in a wide variety of therapeutic areas. Signaling by GPCRs is modulated by the Regulator of G protein Signaling (RGS) protein family. RGS4 modulates insulin release from the pancreas and seizure activity in a variety of epilepsy models and RGS4 is upregulated in neuropathic pain models.
Consequently, inhibition of RGS4 finds use in treating diabetes, epilepsy, depression, neuropathic pain, and other diseases.